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Composition for increasing testosterone levels and enhancing libido

a technology of libido and composition, applied in the direction of pharmaceutical delivery mechanism, food preparation, organic active ingredients, etc., can solve the problems of inconsistent dosing, reduced muscle mass, and decreased circulating testosterone level, so as to increase testosterone levels and enhance libido , the effect of increasing testosterone levels

Inactive Publication Date: 2016-12-15
FARBER MICHAEL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention relates to a formulation and dosage form that can be used to make medicine to increase testosterone levels and enhance libido. The technical effect of this invention is to provide a more effective treatment for men who are struggling with low testosterone levels and sexual dysfunction.

Problems solved by technology

However, after physical maturity, the level of circulating testosterone starts to decline, possibly leading to a diminution in muscle mass.
However, the main problem with such inventions is that they usually end up providing inconsistent dosing because of a great variance in hormone release between the site of injection and the rest of the body.
Because of such uncontrolled release of the active agent, various side-effects developed in periods of high hormone concentrations, such as gynecomastia, water retention, edema and increased fat deposition.
Even if the androgen preparation has shown easy conversion to testosterone in the physiologic environment, it still lacks constant reparation in the organs of predilection and can possibly entail various side-effects.
However, even if conversion to testosterone has been demonstrated as being much more complete than in other cases, the release kinetic of the compound were still not ideal.
However, patients encountered possible risks of developing complications with liver functions, which highly diminishes the convenience of using such technology.
The biggest problem with the administration of flavones and flavanones is their poor absorption characteristics due to enzymatic degradation in the intestine and poor absorption across the intestinal epithelium.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

Preparation of a Formulation #1

[0105]Micronized maltodextrin (micronized powder base) is mixed with micronized powder of 3,4-divanillyltetrahydrofuran and 7-methoxyflavone and 7,8-benzoflavone, which are mixed with desiccated liposomes containing piperine (as a mucosal absorption enhancer). Sweetener and flavoring is added, and the powder is mixed in a fluid bed.

IngredientAmount (g)micronized maltodextrin0.060micronized powder of 3,4-0.040divanillyltetrahydrofuranmicronized 7-methoxyflavone0.040micronized 7,8-benzoflavone0.040desiccated liposomes containing piperine0.0008sweetener0.003flavoring0.004

example 2

Preparation of a Formulation #2

[0106]Micronized maltodextrin (micronized powder base) is mixed with desiccated liposomes containing valine ethyl ester nitrate [VEEN—a compound of formula (I)] and desiccated liposomes containing puerarin extract from pueraria lobata (containing 98% puerarin) are mixed with desiccated liposomes containing piperine (as a mucosal absorption enhancer). Sweetener and flavoring is added, and the powder is mixed in a fluid bed.

IngredientAmount (g)micronized maltodextrin0.080desiccated liposomes of 3,4-0.025divanillyltetrahydrofurandesiccated liposomes of 7-0.020methoxyflavonedesiccated liposomes of 7,8-0.020benzoflavonedesiccated liposomes containing piperine0.0008sweetener0.003flavoring0.004

[0107]Solutions containing the liposomes are sprayed onto the micronized maltodextrin base in a fluid bed. Spraying is effected at a temperature at a nozzle head aperture of about 60° C., and sweetener and flavoring are added.

example 3

Compressed Dosage Forms

[0108]The compressible powder formulation combined with excipients of examples 1 and 2 are compressed into dosage form, which contain individual ingredients in the following amounts:

AmountIngredientmg / dosageDosage form #1micronized maltodextrin60micronized powder of 3,4-40divanillyltetrahydrofuranmicronized 7-methoxyflavone40micronized 7,8-benzoflavone40desiccated liposomes8containing piperinesweetener3flavoring4Microcrystalline cellose90Magnesium stearate9Silicon dioxide6Dosage form #2micronized maltodextrin80desiccated liposomes25containing 3,4-divanillyltetrahydrofurandesiccated liposomes20containing 7-methoxyflavonedesiccated liposomes20containing 7,8-benzoflavonedesiccated liposomes8containing piperinesweetener3flavoring4Microcrystalline cellose73.85Magnesium stearate7.39Silicon dioxide4.92

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Abstract

The present invention features a compressible delivery formulation for buccal delivery, dosage forms and methods of using the same for increasing testosterone levels in a subject. The formulation, dosage forms and methods comprise effective amounts of 3,4-divanillyltetrahydrofuran, 7-methoxyflavone, 7,8-benzoflavone.

Description

BACKGROUND[0001]The subject matter disclosed generally relates to compositions and methods for increasing testosterone levels and enhancing libido, and more particularly to compositions and methods for releasing protein-bound testosterone, and preventing its degradation in vivo.RELATED PRIOR ART[0002]Testosterone is the principal male androgen and is responsible for the development and maintenance of male sexual characteristics, including external virilization, sexual maturity at puberty, spermatogenesis, sexual behaviour, libido and erectile functioning. It also supports bone and muscle tissue development during growth. However, after physical maturity, the level of circulating testosterone starts to decline, possibly leading to a diminution in muscle mass. Therefore, there is a growing need for the development of some form of androgen replacement for the elimination of the effects encountered on muscle mass, which is a specific concern for men evolving in the sports and bodybuildi...

Claims

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Application Information

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IPC IPC(8): A61K9/127A23L1/236A61K9/00A23L1/22A61K31/341A61K31/352
CPCA61K9/127A61K31/341A61K31/352A23V2002/00A23L1/22A23L1/236A61K9/006A61K9/145A23L27/00A23L27/30A61K2300/00
Inventor FARBER, MICHAEL
Owner FARBER MICHAEL
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